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Assay Detail

CHEMBL4345287

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of 6N-FAM from human LRH1 LBD (299 to 541 residues) expressed in Escherichia coli BL21 pLysS by competitive binding based fluorescence polarization assay
9
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor subfamily 5 group A member 2 (CHEMBL3544)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a Versatile and Sensitive Direct Ligand Binding Assay for Human NR5A Nuclear Receptors.
D'Agostino EH, Flynn AR, Cornelison JL, Mays SG, Patel A, Jui NT, Ortlund EA.
ACS Med Chem Lett (2020) 11 : 365 -370
PubMed 32184971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.70 8.68
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4551205 2 8.68
CHEMBL4467442 1 7.19
CHEMBL4288877 1 7.09
CHEMBL1765959 1 6.43
CHEMBL4452196 1 5.62
CHEMBL4448429 1 5.16
CHEMBL259067 1 -
CHEMBL1325149 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4551205 Ki = 2.1 nM 8.68
CHEMBL4467442 Ki = 64.3 nM 7.19
CHEMBL4288877 Ki = 81.4 nM 7.09
CHEMBL1765959 Ki = 374.0 nM 6.43
CHEMBL4452196 Ki = 2400.0 nM 5.62
CHEMBL4448429 Ki = 7000.0 nM 5.16
CHEMBL4551205 Inhibition - % -
CHEMBL259067 Ki - -
CHEMBL1325149 Ki - -